Dihydropolyprenols are a class of known polyprenols that have been found to enhance nonspecific host defenses against a variety of pathogenic microbes in rodents, cows, calves, pigs and swine. Because of their properties of enhancing host resistance, these compounds may be utilized as agents to treat or control infections in animals and human beings.
However, it is becoming increasingly evident that drug development involves much more than merely finding the compound with maximum biological activity. Many other aspects must be considered before a potent active compound can become a medicinal product. Items of high importance are the stability of the active agent, the absorption behavior from the intended site of administration, the physical state of the active agent, and many other related considerations. Economic factors such as the cost of the bulk drug are additional considerations to those of the properties of the active agent itself.
Recognizing these problems, the present invention provides an unexpected oil composition of dihydropolyprenols, which is pharmaceutically elegant and avoids all the problems noted above. This oil composition limits the components to just the vehicle (i.e., oil) and dihydropolyprenols to be efficacious; therefore, it has the potential for a longer shelf-life as there are fewer components interacting with dihydropolyprenols in a detrimental manner. The oil composition also protects dihydropolyprenols from oxidation, a primary degradation pathway for polyprenols, since oxygen would need to diffuse through the oil vehicles to the dihydropolyprenols and more advantageously some oils contain endogenous antioxidants. In addition, physical stability is not a concern with an oil composition since it is a single phase solution. On the other hand, other formulations such as, for example, emulsions disclosed in the related art, are two phases and have the possibility of interreacting each other with time.
The oil composition of the present invention is easy to administer since it can be more concentrated than emulsion formulations, which results in less volume being injected into animals. For example, the emulsion formulation is normally made at 10 mg/mL while our oil based formulation can be at least 150 mg/mL, with a 15-fold reduction in the volume. Also, this oil composition can be easily syringed since the viscosity is low enough for it to flow through a typically used syringe and needle while for example, an implantable pellet containing dihydropolyprenols would be more difficult to administer to animals.
Finally, a simple method is available for manufacturing oil compositions of dihydropolyprenols at a large production size while more complicated and expensive methods are often required for other dosage forms.